Synthesis and properties of a NIR imaging agent that contains boron

Kanser, hücrelerin DNA molekülünde oluşan mutasyonların birikmesiyle, kontrolsüz veya anormal bölünmesi ve çoğalmasıdır. Kanserin tedavisi için birçok yöntem (ameliyat, kemoterapi, radyoterapi vb.) kullanılmaktadır. Bu tedavi yöntemlerinin başında tümörün cerrahi işlem ile alınması gelmektedir. Sağlıklı dokunun hasar görmesini önlemek ve tümörün geride kalıntı bırakmadan alınması son derece önemlidir. Ancak operasyonun başarısı büyük ölçüde operasyonu yürüten cerrahların tecrübe ve yeteneğine bağlı kalabilmektedir. Operasyonun başarı düzeyini arttırmak için son zamanlarda görüntüleme eşliğinde ameliyat yöntemi önerilmiştir. Bu tez çalışmasında yakın kızılötesi bölgede soğurma ve emisyon yapabilen yeni bir boya tasarlanmış ve sentezi gerçekleştirilmiştir. Söz konusu boya tümör hücrelerine kolayca internalize olmak suretiyle kanserli hücrelerin tespit edilmesi maksadıyla kullanılabilecek nitelikte dizayn edilmiştir. Nitekim tez kapsamında yapılan in vitro çalışmalar sonucunda kanser hücrelerinin floresans görüntülemesi gerçekleştirilmiştir. Geliştirilen malzemenin floresans görüntüleme eşliğinde ameliyat işlemlerinde kullanılabileceği düşünülmektedir. Aynı zamanda geliştirilen malzemenin fotoduyarlaştırıcı özelliğiyle in vitro olarak incelenmiş ve başaralı sonuçlar alınmıştır. Üstelik geliştirilen malzeme yüksek oranda bor içermesi münasebeti ile bor nötron yakalama terapisinde (BNYT) ajan olarak kullanılabilecek potansiyele sahiptir.Cancer is the uncontrolled or abnormal division and proliferation of cells with the accumulation of mutations in the DNA molecule. Many methods are used to treat it, one of which is surgical removal of the tumor. It is very important to remove as much tumor as possible and simultaneously to avoid unnecessary damage to healthy tissues. However, the success of the operation may largely depend on the experience and skills of the surgeons performing the operation. In order to increase the success level of the operation, fluorescence guided surgery has been suggested recently. In this thesis it was aimed that synthesized and characterized of a NIR dye that fluorescent in near infrared region. This dye that designed internalized easily with cancer cells. In further studies, tumor cells have been imaged and thought that it can be used in fluorescence guided surgery. At the same time, successful results were seen in in vitro studies with the developed dye photosensitizer feature. Also this dye contains highly amount of boron for potential boron neutron capture therapy (BNCT)

N-doped carbon nanomaterials as fluorescent pH and metal ion sensors for imaging

Herein we describe the facile synthesis of new N-doped carbon nanoparticles (CNPs) obtained from 1,10-phenanthroline by the solvothermal method. Characterization of CNPs were carried out with transmission electron microscope (TEM), X-ray photoelectron spectra (XPS), Fourier transform infrared spectra (FTIR), UV–vis absorption spectra, and luminescence spectra. CNPs were pH sensitive and exploited as fluorescent chemosensors and imaging agents for Al(III) and Zn(II) ions in real-life samples. Remarkably, we show that CNPs can be used for the detection of Al(III) and Zn(II) ions in water samples. Accordingly, the results indicate that CNPs are highly effective in detecting Zn(II) content of cosmetic creams. We also demonstrated that the CNPs could be used for in vitro imaging of Al(III) and Zn(II) in Human Larynx Squamous Cell Carcinoma (Hep-2). Finally, Al(III) imaging in Angelica Officinalis root tissue was also achieved successfully. The CNPs are promising as luminescent multianalyte (pH, Al(III) and Zn(II)) sensors

A generic platform for self-illuminating unimolecular systems enabling photodynamic therapy

This work delineates a generic platform, 1-((1,4-dioxo-1,2,3,4-tetrahydrophthalazin-6-yl)methyl)-1H-1,2,3-triazol-4-yl)methyl 2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoate, (conjugate 1), for self-illuminating unimolecular systems that can both glow in physiological pH (7.4) and enable photodynamic therapy (PDT) in highly acidic environments. It is noteworthy that conjugate 1 induces chemiluminescence upon treatment with KO2 at physiological pH. Also, it is remarkable that this straightforward design effectively boosts the singlet oxygen generation. Most strikingly, conjugate 1 can function as a photosensitizer even in highly acidic environments. Crucially, conjugate 1 shows in vitro phototoxicity when illuminated for 30 min. Furthermore, the capability of conjugate 1 as a self-illuminating PDT agent is explored. To our delight, we noted that conjugate 1 can eliminate 79% of cancerous cells upon chemical excitation being triggered in vitro. The data render its efficiency as a self-illuminating anticancer therapy agent. Last but not least, conjugate 1 can successfully inhibit the growth of bacteria. Also, we found that the shelf life of the acidic beverages can be extended from 2 days to ≅ 6–7 days after photodynamic sterilization with conjugate 1. To our best knowledge, this is the first example of luminol-based self-illuminating unimolecular systems enabling PDT for anticancer and antibacterial activities

Norsquaraine endowed with anticancer and antibacterial activities

Photodynamic therapy (PDT) is a method for the treatment of cancer. Furthermore, PDT can also be used for the eradication of bacteria. The photo-sensitizing drug, a.k.a photosensitizer, is critical for the success of PDT. Although norsquaraines are analogs of squaraine dyes, they are overlooked as photosensitizers. Methods: In this work, synthesis, characterization, bioimaging and in vitro PDT applications of a new norsquaraine dye 1 were described. We also prepared nanoparticles from norsquaraine 1 and Pluronic F127 to obtain 1@F127. Results: Norsquaraine 1 boosted the generation of reactive oxygen species over a wide range of pH (pH 8.0, 7.0, 6.0, and 2.2.). Furthermore, 1 was internalized by epidermoid laryngeal carcinoma Hep-2 (Hep-2) cells and used for fluorescence imaging. Remarkably, norsquaraine 1 destroyed most of the cancer cells (ca. 77% to 89%) after illumination with red light. Most strikingly, 1 successfully inhibited the growth of Methicillin-resistant Staphylococcus aureus (MRSA) upon illumination. Last but not least, photodynamic sterilization of tomato juice, an acidic beverage, was feasible using 1 as a photo sterilizer. Nano formulation of 1 with Pluronic F127 provided 1@F127 nanoparticles. It is lucid that 1@F127 nanoparticles permeate into Hep-2 cells and boost the generation of ROS upon illumination. Conclusion: Norsquaraine 1 shows superior features as a photosensitizer pertinent to PDT in a wide range of pH. This norsquaraine is endowed with anticancer and antibacterial activities. Which should be further evaluated